Krogsgaard-Larsen, N.Jensen, A.Schrøder, T.Christoffersen, C.Kehler, J.2016-10-192016-10-192014Journal of Medicinal Chemistry, 2014; 57(13):5823-58280022-26231520-4804http://hdl.handle.net/2440/101916Niels Krogsgaard-Larsen, Anders A. Jensen, Tenna J. Schroder, Claus. T. Christoffersen and Jan KehlerBy introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar receptor binding affinities for the dopamine D₂ and serotonin 5-HT₆ receptor subtype, respectively. While the 5-HT₆ ligands were antagonists, the D₂ ligands displayed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity. These structures could potentially be interesting for treatment of neurological diseases such as schizophrenia, Parkinson's disease, and cognitive deficits.enErgolinesNovel Aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligandsNovel Aza-analogous ergoline derived scaffolds as potent serotonin 5-HT(6) and dopamine D(2) receptor ligandsJournal article003001563410.1021/jm50037590003389791000262-s2.0-8490428894494237